Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes

Balseven H., Isgor M. M., Mert S., Alim Z., BEYDEMİR Ş., Ok S., ...More

BIOORGANIC & MEDICINAL CHEMISTRY, vol.21, no.1, pp.21-27, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 21 Issue: 1
  • Publication Date: 2013
  • Doi Number: 10.1016/j.bmc.2012.11.012
  • Journal Name: BIOORGANIC & MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Page Numbers: pp.21-27
  • Anadolu University Affiliated: No

Abstract

In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, H-1 NMR, C-13 NMR and LC-MS analysis. H-1 NMR and C-13 NMR revealed the tautomeric structures. hCA I and hCA II isozymes were purified from human erythrocytes and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied. The K-i values of compounds were 0.062-1.278 mu M for hCA I and 0.012-0.379 mu M for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range. Published by Elsevier Ltd.